Lead Compound
Our initial product candidate is Difluoro-Etoposide™ (Adva-27a), a Carbon-Difluoride derivative of Etoposide, targeted for various forms of cancer. Difluoro-Etoposide™ is expected to enter Phase I clinical trials in Canada later this year. Etoposide, also commonly known as Vepesid or VP-16, is currently on the market and has been for over 20 years. It is sold under different brand names by various drug companies including, VePesid, Etopophos and Vumon or Teniposide (Bristol-Myers Squibb), Toposar (Sicor/Pfizer), Lastet (Nippon Kayaku Ltd) and Etoposide (TEVA, Bedford Laboratories, Supergen, American Pharmaceutical Partners, Watson Pharmaceuticals, and Genpharm). Etoposide is an effective anti-tumor compound and is currently in use to treat various types of cancer including leukemia, lymphoma, testicular cancer, breast cancer, lung cancer, brain cancer, prostate cancer, bladder cancer, colon cancer, ovarian cancer, liver cancer and several other forms of cancer. It is also being tested in clinical trials against other types of cancer, such as Kaposi's sarcoma. Etoposide is administered both intravenously and orally as liquid capsules. It has the following chemical structure:
This Etoposide compound which is currently in use suffers from molecular instability leading to reduced efficacy and high toxicity. Using our Carbon-Difluoride platform technology, we constructed several Difluoro derivatives of Etoposide by replacing the labile diester bond between the sugar and the toxin moieties of the existing Etoposide molecule with a Carbon-Difluoride bond. All Difluoro substituted constructs were found to be completely stable. We subsequently tested these constructs for their ability to kill cancer cells in vitro by conducting side-by-side experiments against the standard Etoposide compound. The results of these studies, which have been published in our patent application show that several constructs have retained activity. One of such constructs, Adva-27a, showed enhanced cancer cell killing activity over the existing Etoposide molecule. This new compound, which we call Difluoro-Etoposide™, is entering Phase I clinical trials in Canada later this year. The planned clinical trials for small-cell lung cancer indication will be carried out at the Jewish General Hospital, one of the McGill University Hospital Centers in Montreal (Canada). In addition, we are planning to conduct Phase I clinical trials on Multi-Drug-Resistant breast cancer patients at Hotel Dieu Hospital, one of the University of Montreal Hospital Centers. All aspects of the planned clinical trials in Canada will employ FDA standards at all levels.
The following is a space-filling model of our Lead Compound, Difluoro-Etoposide™ (Adva-27a):
